| Identification | Back Directory | [Name]
N-methyl-3-(1-(4-(piperazin-1-yl)phenyl)-5-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazol-3-yl)propanamide | [CAS]
1333146-24-9 | [Synonyms]
CS-4936
CS-2064
OSU-T315
GTPL8116
ILK-IN-1
BDBM50353484
CHEMBL1830587
SCHEMBL8536228
ILK-IN-2 (CPD 22: OSU-T315 analog)
1H-Pyrazole-3-propanamide, N-methyl-1-[4-(1-piperazinyl)phenyl]-5-[4'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]-
N-methyl-3-(1-(4-(piperazin-1-yl)phenyl)-5-(4'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)-1H-pyrazol-3-yl)propanamide | [Molecular Formula]
C30H30F3N5O | [MDL Number]
MFCD29472239 | [MOL File]
1333146-24-9.mol | [Molecular Weight]
533.59 |
| Chemical Properties | Back Directory | [Boiling point ]
739.2±60.0 °C(Predicted) | [density ]
1.27±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 10mM | [form ]
A solid | [pka]
16.02±0.46(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
ILK-IN-2 (OSU-T315 analog) is an oral PDK2 inhibitor and also an ILK inhibitor, with an IC50 of 0.6 μM. ILK-IN-2 induces cell autophagy and apoptosis, showing anti-tumor activity. ILK-IN-2 directly abolishes AKT activation by preventing AKT from translocating to lipid rafts, triggering Caspase-dependent apoptosis in chronic lymphocytic leukemia (CLL) and extending the lifespan in TCL1 mouse models[1][2]. | [in vivo]
ILK-IN-2 (25-50 mg/kg, oral or intraperitoneal injection, once daily, 2-4 weeks) delays leukemia progression in mice and significantly improves the overall survival rate of mice harboring TCL1 leukemia cells[ 1 ].
ILK-IN-2 (25-50 mg/kg, orally, daily, for 35 days) inhibits the growth of PC-3 xenograft tumors in nude mice[2]. | Animal Model: | Pharmacokinetic properties of OSU-T315[1] | | Dosage: | 50 mg/kg, daily for 4 weeks; 25 mg/kg, once daily for 2 weeks | | Administration: | Oral; Intraperitoneal injection (i.p.) | | Result: | Reduced white blood cell count and prolonged the survival of mice. |
| Animal Model: | PC-3 tumor xenograft mice model[2] | | Dosage: | 25, 50 mg/kg; daily; 35 days | | Administration: | Oral | | Result: | Significantly inhibited tumor growth (25 and 50 mg/kg groups inhibited 48% and 62% respectively).
Showed that the phosphorylation of Ser-473-Akt was dose-dependently inhibited, while the phosphorylation of Thr-308-Akt was not affected. At the same time, the phosphorylation levels of GSK3β and MLC and the expression levels of YB-1, HER2 and EGFR also appeared in parallel decline.
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| [IC 50]
ILK: 0.6 μM (IC50) | [storage]
Store at -20°C | [References]
[1] Ta-Ming Liu, et al. OSU-T315: a novel targeted therapeutic that antagonizes AKT membrane localization and activation of chronic lymphocytic leukemia cells. Blood. 2015 Jan 8;125(2):284-95. DOI:10.1182/blood-2014-06-583518
[2] Su-Lin Lee, et al. Identification and characterization of a novel integrin-linked kinase inhibitor. J Med Chem. 2011 Sep 22;54(18):6364-74. DOI:10.1021/jm2007744 |
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